Dopamine Receptor
Dopamine receptors are GPCRs through which dopamine regulates motor function, motivation, drive, cognition, and peripheral physiology[1][2]. Mechanistically, dopamine receptor signaling is organized into D1-like receptors (D1, D5) and D2-like receptors (D2S, D2L, D3, D4), enabling subtype-specific control of cAMP-mediated and non-canonical signaling[1][3]. In disease-oriented research, dopamine-glutamate-NMDA interactions and dopamine receptor ligands provide experimental frameworks for schizophrenia, Parkinson’s disease, depression, bipolar disorder, and addiction models[1][3]. Compared with related isoforms, D1-D2 receptor heteromers form a pharmacologically distinct signaling complex coupled to Gq/11, requiring agonist binding to both receptors for G protein activation and intracellular calcium release[4]. This calcium pathway links D1-D2 receptor heteromer activation to CaMKIIα, BDNF production, and neuronal growth in striatal models[5]. Compared with D1, D5 shows high agonist affinity and constitutive activity shaped by carboxyl-terminal tail sequence and intracellular loop determinants[6][7]. Therefore, subtype-selective agonists, antagonists, partial agonists, and heteromer-directed ligands remain practical tools for dissecting dopamine receptor pharmacology, signaling bias, and disease-relevant neurocircuit mechanisms[1][3][4].
References:
- [1]. Martel JC, et al. Dopamine Receptor Subtypes, Physiology and Pharmacology: New Ligands and Concepts in Schizophrenia. Front Pharmacol. 2020 Jul 14;11:1003. [Content Brief]
- [2]. Beaulieu JM, et al. The physiology, signaling, and pharmacology of dopamine receptors. Pharmacol Rev. 2011 Mar;63(1):182-217. [Content Brief]
- [3]. Beaulieu JM, et al. Dopamine receptors - IUPHAR Review 13. Br J Pharmacol. 2015 Jan;172(1):1-23. [Content Brief]
- [4]. Rashid AJ, et al. D1-D2 dopamine receptor heterooligomers with unique pharmacology are coupled to rapid activation of Gq/11 in the striatum. Proc Natl Acad Sci U S A. 2007 Jan 9;104(2):654-9. [Content Brief]
- [5]. Hasbi A, et al. Calcium signaling cascade links dopamine D1-D2 receptor heteromer to striatal BDNF production and neuronal growth. Proc Natl Acad Sci U S A. 2009 Dec 15;106(50):21377-82. [Content Brief]
- [6]. Demchyshyn LL, et al. Dopamine D5 receptor agonist high affinity and constitutive activity profile conferred by carboxyl-terminal tail sequence. J Biol Chem. 2000 Aug 4;275(31):23446-55. [Content Brief]
- [7]. Tumova K, et al. Role of the fourth intracellular loop of D1-like dopaminergic receptors in conferring subtype-specific signaling properties. FEBS Lett. 2004 Oct 22;576(3):461-7. [Content Brief]
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Dopamine Receptor Ligands
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Dopamine Receptor Related Products (537)
Related Products (537)
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Pericyazine (Standard)
0 ImagesSynonyms: Propericiazine (Standard); RP 8909 (Standard)Pericyazine (Standard) is the analytical standard of Pericyazine. This product is intended for research and analytical applications. Pericyazine (Propericiazine) is a first-generation antipsychotic agent that is used as an adjunct to the short-term management of severe anxiety states and psychosis. Pericyazine is a selective D2-dopamine receptor antagonist. Pericyazine has adrenolytic, anticholinergic, and extrapyramidal effects.
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S-14506 hydrochloride (Standard)
0 ImagesCat. No.: HY-110024RCAS No.: 286369-38-8S-14506 hydrochloride (Standard) is the analytical standard of S-14506 (hydrochloride) (HY-110024). This product is intended for research and analytical applications. S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocKing dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.
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(±) Anabasine hydrochloride
0 ImagesCat. No.: HY-W209279CAS No.: 352220-15-6(±) Anabasine hydrochloride is the racemic form of Anabasine (HY-B1532). (±) Anabasine hydrochloride stimulates the release of [3H]-Dopamine from mouse striatal synaptosomes. (±) Anabasine hydrochloride inhibits the high-affinity binding of [3H]-S-(-)-Nicotine to the striatal membrane. Anabasine hydrochloride is an agonist of α7nAChR and possesses anti-inflammatory and insecticidal activities.
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Ropinirole-d3 hydrochloride
0 ImagesCat. No.: HY-B0623AS2CAS No.: 1329611-00-8Synonyms: SKF 101468-d3 hydrochlorideRopinirole-d3 hydrochloride is the deuterium labeled Ropinirole hydrochloride. Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
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ADR 851 free base
0 ImagesCat. No.: HY-101747CAS No.: 138559-56-5ADR 851 free base is a dopamine D2 receptor antagonist,and can be used in research on antiemetics.
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Oxidopamine hydrochloride (Standard)
0 ImagesCat. No.: HY-B1081RCAS No.: 28094-15-7Synonyms: 6-Hydroxydopamine Hydrochloride (Standard)Oxidopamine hydrochloride (Standard) is the analytical standard of Oxidopamine hydrochloride (HY-B1081). This product is intended for research and analytical applications. Oxidopamine (6-OHDA) hydrochloride is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrochloride is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrochloride promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytoKine IL-1β secretion. Oxidopamine hydrochloride can be used for the research of ParKinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.
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(Rac)-Rotigotine hydrochloride (Standard)
0 ImagesSynonyms: N-0437 hydrochloride (Standard)(Rac)-Rotigotine (hydrochloride) (Standard) is the analytical standard of (Rac)-Rotigotine (hydrochloride). This product is intended for research and analytical applications. (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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Thiethylperazine-d3
0 ImagesCat. No.: HY-B1794SThiethylperazine-d3 is the deuterium labeled Thiethylperazinee (HY-B1794). Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.
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SKF-80723
0 ImagesCat. No.: HY-137254CAS No.: 71636-62-9SKF-80723 is a D1 receptor agonist and can be used for study of Parkinson's disease.
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Pentiapine (Standard)
0 ImagesCat. No.: HY-100143RCAS No.: 81382-51-6Synonyms: CGS 10746 (Standard)Pentiapine (Standard) is the analytical standard of Pentiapine (HY-100143). This product is intended for research and analytical applications. Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites.
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Foscarbidopa (Standard)
0 ImagesCat. No.: HY-109131RCAS No.: 1907685-81-7Synonyms: ABBV-951 (Standard); Carbidopa 4′-monophosphate (Standard)Foscarbidopa (Standard) is the analytical standard of Foscarbidopa (HY-109131). This product is intended for research and analytical applications. Foscarbidopa (ABBV-951; Carbidopa 4′-monophosphate) is a proagent of Carbidopa, acts as a dopamine receptor agonist.
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Lumateperone (Standard)
0 ImagesSynonyms: ITI-007 (Standard)Lumateperone (Standard) is the analytical standard of Lumateperone. This product is intended for research and analytical applications. Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression.
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Aplindore fumarate
0 ImagesCat. No.: HY-129507CAS No.: 189681-71-8Synonyms: DAB-452 fumarateAplindore fumarate (DAB-452 fumarate) is a dopamine D2 receptor partial agonist. Aplindore fumarate could be used in studies of Parkinson's disease and schizophrenia.
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L 646462
0 ImagesCat. No.: HY-118209CAS No.: 89149-85-9L-646462 is an antagonist of dopamine and 5-HT, with selectivity for the peripheral system (the central/peripheral activity ratio of L-646462 is 143). L-646462 can be used in research related to nausea, vomiting, and associated neurological disorders.
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Itopride-d6
0 ImagesCat. No.: HY-B0732ASCAS No.: 1346746-82-4Synonyms: HSR803-d6 free baseItopride-d6 (HSR803-d6 (free base)) is deuterium labeled Itopride. Itopride (HSR803 free base) is a potent and orally active dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
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Hydrastine (Standard)
0 ImagesSynonyms: (-)-β-Hydrastine (Standard); (1R,9S)-β-Hydrastine (Standard)Hydrastine (Standard) is the analytical standard of Hydrastine (HY-B0927). This product is intended for research and analytical applications. Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) is a selective competitive inhibitor of tyrosine hydroxylase (TH), inhibiting dopamine biosynthesis (IC50=20.7 μM, PC12 cells). Hydrastine also inhibits the organic cation transporter OCT1 (IC50=6.6 μM). Hydrastine may cause neuronal toxicity through mitochondrial dysfunction rather than oxidative stress damage, and can aggravate cell apoptosis when combined with L-DOPA. Hydrastine can be used to study Parkinson's disease-related dopaminergic neuronal damage.
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Fenoldopam mesylate (Standard)
0 ImagesSynonyms: Fenoldopam methanesulfonate (Standard); SKF-82526 mesylate (Standard)Fenoldopam mesylate (Standard) is the analytical standard of Fenoldopam mesylate (HY-B0735A). This product is intended for research and analytical applications. Fenoldopam (SKF-82526) mesylate is a selective dopamine D1 receptor agonist. Fenoldopam mesylate binds to rat D1B dopamine receptors (Kd = 11 nM) and human D1A receptors (Kd = 17 nM) in COS-7 cell membranes expressing the cloned receptors. Fenoldopam mesylate modulates dopamine receptor expression, induces vasorelaxation in vascular tissues, reverses glomerular hyperfiltration in rat models, increases intracellular cAMP levels, promotes DARPP-32 phosphorylation in small cell lung cancer (SCLC) cells, inhibits cytokine secretion, and downregulates T cell activation markers in activated human T cells. Fenoldopam mesylate can be used for research on hypertension, acute kidney injury, psoriasis, and small cell lung cancer.
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Ziprasidone (Standard)
0 ImagesSynonyms: CP-88059 (Standard)Ziprasidone (Standard) is the analytical standard of Ziprasidone. This product is intended for research and analytical applications. Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
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Fananserin (Standard)
0 ImagesCat. No.: HY-103104RCAS No.: 127625-29-0Synonyms: RP 62203 (Standard)Fananserin (Standard) is the analytical standard of Fananserin (HY-103104). This product is intended for research and analytical applications. Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
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(±) Anabasine (Standard)
0 Images(±) Anabasine (Standard) is the analytical standard of (±) Anabasine (HY-W052144). This product is intended for research and analytical applications. (±) Anabasine is the racemic form of Anabasine (HY-B1532). (±) Anabasine stimulates the release of [3H]-Dopamine from mouse striatal synaptosomes. (±) Anabasine inhibits the high-affinity binding of [3H]-S-(-)-Nicotine to the striatal membrane. Anabasine is an agonist of α7nAChR and possesses anti-inflammatory and insecticidal activities.
